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1. (WO2007007628) CHOLINE SALT CRYSTAL OF AZULENE COMPOUND
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2007/007628    International Application No.:    PCT/JP2006/313468
Publication Date: 18.01.2007 International Filing Date: 06.07.2006
IPC:
C07D 309/10 (2006.01), A61K 31/351 (2006.01), A61P 3/10 (2006.01), C07C 215/90 (2006.01)
Applicants: ASTELLAS PHARMA INC. [JP/JP]; 3-11, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo 1038411 (JP) (For All Designated States Except US).
KOTOBUKI PHARMACEUTICAL CO., LTD. [JP/JP]; 6351, Oaza-Sakaki, Sakaki-machi, Hanishina-gun, Nagano 3890697 (JP) (For All Designated States Except US).
IMAMURA, Masakazu [JP/JP]; (JP) (For US Only).
SUZUKI, Takayuki [JP/JP]; (JP) (For US Only).
MURAKAMI, Takeshi [JP/JP]; (JP) (For US Only).
NAKANISHI, Keita [JP/JP]; (JP) (For US Only).
UEBAYASHI, Hiroshi [JP/JP]; (JP) (For US Only).
NAKAMURA, Haruka [JP/JP]; (JP) (For US Only).
YUDA, Masamichi [JP/JP]; (JP) (For US Only).
AMENOMIYA, Naoko [JP/JP]; (JP) (For US Only).
AWAMURA, Yuuji [JP/JP]; (JP) (For US Only).
TOMIYAMA, Hiroshi [JP/JP]; (JP) (For US Only)
Inventors: IMAMURA, Masakazu; (JP).
SUZUKI, Takayuki; (JP).
MURAKAMI, Takeshi; (JP).
NAKANISHI, Keita; (JP).
UEBAYASHI, Hiroshi; (JP).
NAKAMURA, Haruka; (JP).
YUDA, Masamichi; (JP).
AMENOMIYA, Naoko; (JP).
AWAMURA, Yuuji; (JP).
TOMIYAMA, Hiroshi; (JP)
Agent: WATANABE, Kazuhira; 3rd Fl., No.8 Kikuboshi Tower Building, 20-18, Asakusabashi 3-chome, Taito-ku, Tokyo 1110053 (JP)
Priority Data:
2005-198973 07.07.2005 JP
Title (EN) CHOLINE SALT CRYSTAL OF AZULENE COMPOUND
(FR) CRISTAL DE SEL DE CHOLINE DE COMPOSE AZULENE
(JA) アズレン系化合物のコリン塩結晶
Abstract: front page image
(EN)A choline salt crystal of (1S)-1,5-anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]- D-glucitol which shows an endothermic peak at 194 to 198°C as measured by differential scanning calorimetry (DSC analysis) and shows main peaks at about 2&thetas;(°) 5.58, 14.72, 16.80, 17.82, 21.02 and 22.46 as measured by powder X ray diffraction. Thus, a crystal of an azulene compound can be produced which is in the form of a single crystal, has a fixed quality, can be produced with good reproducibility, can be provided stably as a crystal of an active substance for use in the preparation of a pharmaceutical and is excellent in storage stability.
(FR)L'invention concerne un cristal de sel de choline de (1S)-1,5-anhydro-1-[5-(azulèn-2-ylméthyl)-2-hydroxyphényl]-D-glucitol présentant un pic endothermique à une température comprise entre 194 °C et 198 °C sur la base d'une analyse calorimétrique différentielle (analyse ACD) et des pics principaux sur une échelle 2$g(u)(°) à 5,58, 14, 72, 16,80, 17,82, 21,02 et 22,46 environ, sur la base d'une analyse par diffraction de rayons X sur poudres. L'invention permet ainsi de produire un cristal d'un composé d'azulène sous forme de monocristal, possédant une qualité fixe, pouvant être produit en série, fourni de façon stable sous forme de cristal d'une substance active, utilisé dans la préparation d'un produit pharmaceutique, et possédant une excellente stabilité de conservation.
(JA) 示差走査熱量計分析(DSC分析)で194~198°Cに吸熱ピークを有するとともに、粉末X線回折で2θ(°)5.58、14.72、16.80、17.82、21.02及び22.46付近に主ピークを有する、(1S)-1,5-アンヒドロ-1-[5-(アズレン-2-イルメチル)-2-ヒドロキシフェニル]-D-グルシトールのコリン塩結晶とすることにより、一定の品質を有する単一の結晶が再現性よく得られ、医薬の製造に用いられる原薬の結晶として安定的に供給されることが可能で、かつ、保存安定性に優れたアズレン系化合物の結晶が提供される。
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)